Endothelin receptor

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Endothelin receptor is a type of G protein-coupled receptor that is activated by the protein endothelin. There are two types of endothelin receptors: ETA and ETB. These receptors play a crucial role in vasoconstriction, cell proliferation, and neurotransmission.

Structure[edit | edit source]

Endothelin receptors are integral membrane proteins that contain seven transmembrane domains, which is a common characteristic of G protein-coupled receptors. The ETA and ETB receptors share a 63% amino acid sequence identity.

Function[edit | edit source]

Endothelin receptors are found in various tissues, including the vascular smooth muscle, heart, lung, and kidney. They are involved in a variety of physiological processes.

ETA Receptor[edit | edit source]

The ETA receptor primarily mediates vasoconstriction and cell proliferation. It is predominantly found in vascular smooth muscle cells. Activation of the ETA receptor by endothelin leads to vasoconstriction and cell proliferation.

ETB Receptor[edit | edit source]

The ETB receptor has a dual role. It is located in the endothelial cells where it mediates vasodilation by releasing nitric oxide and prostacyclin. It is also found in smooth muscle cells where it mediates vasoconstriction.

Clinical significance[edit | edit source]

Endothelin receptors have been implicated in a variety of diseases, including pulmonary arterial hypertension, heart failure, and cancer. Antagonists of the endothelin receptor, such as bosentan, ambrisentan, and macitentan, are used clinically to treat pulmonary arterial hypertension.

See also[edit | edit source]

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Contributors: Prab R. Tumpati, MD